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Key Documents

SML0895

Sigma-Aldrich

AGI-6780

≥98% (HPLC)

Sinônimo(s):

N-Cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide

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About This Item

Fórmula empírica (Notação de Hill):
C21H18F3N3O3S2
Número CAS:
1432660-47-3
Peso molecular:
481.51
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

cor

white to light brown

solubilidade

DMSO: 20 mg/mL, clear

temperatura de armazenamento

2-8°C

InChI

1S/C21H18F3N3O3S2/c22-21(23,24)14-2-1-3-16(10-14)25-20(28)26-19-11-17(32(29,30)27-15-4-5-15)6-7-18(19)13-8-9-31-12-13/h1-3,6-12,15,27H,4-5H2,(H2,25,26,28)

chave InChI

CCAWRGNYALGPQH-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.

Características e benefícios

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

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Jan Mauer et al.
Nature chemical biology, 15(4), 340-347 (2019-02-20)
Small nuclear RNAs (snRNAs) are core spliceosome components and mediate pre-mRNA splicing. Here we show that snRNAs contain a regulated and reversible nucleotide modification causing them to exist as two different methyl isoforms, m1 and m2, reflecting the methylation state
Kancharana Bala Bhaskara Rao et al.
FEBS letters, 593(16), 2177-2193 (2019-06-19)
Isocitrate dehydrogenases (IDHs) are metabolic enzymes that are mutated in several cancers, resulting in overproduction of d-2-hydroxyglutarate (D-2HG). However, the signalling pathways and factors that regulate mutant IDHs or their metabolites remain elusive. Here, we report that in synchronized cells

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